RT Journal Article
SR Electronic
T1 Imaging the Activity of Efflux Transporters at the Blood–Brain Barrier in Neurologic Diseases: Radiotracer Selection Criteria
JF Journal of Nuclear Medicine
JO J Nucl Med
FD Society of Nuclear Medicine
SP jnumed.124.269322
DO 10.2967/jnumed.124.269322
A1 Tournier, Nicolas
A1 Langer, Oliver
YR 2025
UL http://jnm.snmjournals.org/content/early/2025/02/27/jnumed.124.269322.abstract
AB Efflux transporters of the adenosine triphosphate–binding cassette (ABC) superfamily, such as P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2), are highly expressed at the blood–brain barrier (BBB), where they contribute to maintaining brain homeostasis. P-gp may serve as an imaging biomarker to assess the contribution of BBB functionality rather than integrity to the onset or progression of various neurologic diseases. Considerable efforts have been made to develop radiolabeled P-gp substrates to assess cerebral P-gp activity with PET. However, initially developed radiotracers have limited clinical utility as they lack sensitivity to detect moderate, physiologically relevant changes in cerebral P-gp activity. Learning from this molecular imaging area has called for specific criteria, different from those classically used for other central nervous system targets, for developing and selecting suitable PET tracers to study ABC transporter activity at the BBB in different neurologic diseases.